SB-612111 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性阿片受体样孤儿受体 (ORL-1、NOP) 拮抗剂，Ki 为 0.33 nM。

A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM; displays good selectivity versus mu-(174-fold), delta-(6391-fold), and kappa (486-fold)-opioid receptors; antagonizes the antimorphine action of nociceptin (ED50= 0.69 mg/kg) with no measurable antinociceptive effects in vivo; antagonizes nociceptin-induced thermal hyperalgesia (ED50=0.62 mg/kg i.v.) in rat carrageenan inflammatory pain model.

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rel-SB-612111 hydrochloride (intravenous?injection; 0.6-10 nmol/mouse)antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg.rel-SB-612111 hydrochloride (intravenous?injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected. Animal Model:Male rats Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg Administration:Intravenous?injection; single dose Result:Had antihyperalgesic effects on carrageenan-induced rat paw.

SB 612111 | SB612111

Endocrinology/Hormones

Opioid Receptor

Opioid Receptor

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371980-94-8

454.86

C24H29Cl2NO.HCl

>98% (HPLC)

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CC1=C2CCC(CC(C2=CC=C1)O)CN3CCC(CC3)C4=C(C=CC=C4Cl)Cl.Cl

7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years